Building Blocks

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

N-Carbobenzoxypropargylamine (CBPA) is an isoxazole that has been shown to bind to the integrin receptor, which is a type of protein found on the surface of cells. CBPA binds to the ligand-binding site of the integrin receptor and inhibits its activation by connecting it with a peptide fragment. This results in a loss of cell adhesion and reduced proliferation. CBPA has a nanomolar range and can be used as a potential drug candidate for cancer treatment because it has high affinity for cells and high frequency of occurrence. The pharmacophore model for CBPA was generated using aspartic acid, which is one of the most abundant amino acids in proteins.

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

3-Methyl-1,2,3,4-tetrahydroquinoline is a synthetic molecule that has been shown to have adjuvant activity in the treatment of cancer. 3-Methyl-1,2,3,4-tetrahydroquinoline inhibits bacterial growth by alkylating DNA and RNA. It binds to nucleic acids and prevents transcription and replication. The molecular structure of 3-methyl-1,2,3,4-tetrahydroquinoline was elucidated by FTIR spectroscopy and XRPD analysis. This compound has also been shown to inhibit the growth of Staphylococcus aureus strains.

1-(2-Methoxy-5-methylphenyl)ethanone is a volatile, synthetic compound. It is used as a chemical intermediate in the production of picotamide and esterification products. Methoxyphenylacetic acid (1) is methylated with methanol in the presence of hydrochloric acid to form 2,5-dimethoxybenzoic acid (2). The latter is then esterified with methanol and acetic anhydride to yield picotamide (3).

Versatile small molecule scaffold

Versatile small molecule scaffold

Versatile small molecule scaffold

5-Methoxy-benzo[b]thiophene is a synthetic compound that has been shown to have antiestrogenic activity. It was synthesized using the acetonitrile technique and has been shown to inhibit the growth of mammary carcinomas in mice. 5-Methoxy-benzo[b]thiophene binds to estrogen receptor protein, which inhibits the binding of estrogen and prevents its effects on breast cancers. This agent also has been shown to be an effective therapy for some human breast cancer cells, which may be due to its ability to block estrogen receptor function.

1,1-Dioxido-1-benzothien-6-ylamine is a cytotoxic drug that inhibits the synthesis of DNA and RNA in cancer cells. It is synthesized from benzo[c]thiophene-2,5-dione by oxidation with nitric acid to give the corresponding dioxido compound. The synthesized product has high lipophilicity (log P = 2.2) and a reactive hydroxy group that can undergo modifications such as esterification or alkylation. 1,1-Dioxido-1-benzothien-6-ylamine shows potent antitumor activity against solid tumours and high lipophilicity that enables it to cross the blood brain barrier very easily. It also induces apoptosis in tumour cells by binding to nucleic acids and inhibiting their synthesis. This drug is cytotoxic at nanomolar concentrations and has been shown to be effective against lung